Anti Hypertensive

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Anti Hypertensive
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Anti Hypertensive

• Types of HTN
• Alternate HTN.
• Mild HTN (DBP 91 -104 MMHg).
• Moderate HTN (DBP 105 -114 MMHg).
• Severe HTN (DBP lt 115 MMHg without End organ
  damage).
• Malignant HTN (DBP lt 115 MMHg with end organ
  damage).
• Systolic HTN (syst BP lt 160 MMHg(

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ANTI HYPERTENSIVE THERAPY

• Diuretics- 4 major groups
• Carbonic anhydrase inhibitors (prox. Tubules)
• 2. Loop Diuretics
  Dose
• Bumetanide (Bumex) 0.5 5 mg
• Ethacrynic acid (Edecrin) 25 100 mg
• Furosemide (Lasix) 40 480 mg

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3. Thiazides and Related Sulfonamide Comp.

• Chlorothiazide (Diuril) 125 500 mg
• Cyclothiazide (Anhydron) 0.5 2mg
• Hydrochlorothiazide (Esidrix) 12.5 50 mg
• Polythiazide (Renese) 1 4 mg
• Methylclothiazide (Enduron) 2.5 5 mg
• Bendroflumethiazide (Naturetin) 2.5 5 mg
• Benzthiazide (Aquatag) 12.5 50 mg
• Triclormethiazide (Metahydrin) 1 4 mg

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Sulfonamide Compounds

• Chlorthalidone (Hygroton) 12.5 -50 mls
• Indapamide (Lozol) 2 5 mg
• Metolazone (Zaroxolyn) 1 - 10 mg
• Quinethazone (Hydromox) 25 100 mg
• 4. Potassium Sparing Agents
• Spironolactone (Aldactone) 25 100 mg
• Amiloride (Midamor) 5 10 mg
• Triamterene (Dyrenium) 50 100 mg

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MECHANISMS BY WHICH CHRONIC DIURETIC THERAPY MAY
LEAD TO VARIOUS COMPLICATIONS

• 
  Diuretic therapy
• Renal reabsorption of Na (and Mg)
  Hypomagnesemia
• Hyponatremia Saluresis and
  dluresis
• 
  Plasma volume
• Cardiac output Renal blood flow
  PRA
• Postural hypotension GFR
  Aldosterone
• 
  Pre-renal Proximal
  Distal Ca Kaliuresis
• azotemia
  reabsorption reabsorption
• 
  uric acid calcium
  Hypokalemia
  Hyper

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Dosage and Choice of Agent

• Mild Moderate HTN
• With serum creatinine gt 2 mg/dL
• With serum creatinine lt 2 mg/dL

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Side Effects

• Hypolemia
• Use small dose of diuretics.
• Use moderately long acting (1218 hours).
• Restrict Na intake.
• Increase dietary K intake.
• Restrict use of laxative.
• Combined Thiazide with K sparing agent.

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Side Effects (cont.)

• 2. Hyponatremia
• 3. Hypomagnesemia
• 4. Hyperuricemia
• 5. Hypercholesterolemia
• 6. Hypercalcemia
• 7. Hyperglycemia
• 8. Impotence
• 9. Use of NSAIDs

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Adrenergic Inhibitors

• Peripheral Inhibitors
• Reserphine
• Guanethidine (Ismelin)
• Guanadrel (Hylorel)
• Bethanidine (Tenathan)
• Central Inhibitors
• Methyldopa (Aldomet)
• Clonidine (Catapres)

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A- Receptor Blockers

• a1- Receptor
• Doxazosin ( Cardura)
• Prazosin (Minipress)
• B. a1 and a2- Receptors
• Phentolamine (Regitine)
• Phenoxybenzamine (Dibenzyline)

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B- Receptor Blockers

• Acebutolol (Sectral)
• Atenolol (Ternomin)
• Betaxolol (Kerlone)
• Metoprolol (Lopressor)
• Nadolol (Corgard)
• Penbutolol (Levatol)
• Pindolol (Visken)
• Propranolol (Inderal)

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Beta-adrenoceptor blocking drugs

• Nonselective selective
  with alpha-blocking
• 
  
  activity
• - -
  Labetalol
• ISA ISA ISA
  ISA Bucindolol
• 
  
  Carvedilol
• Nadolol Pindolol Atenolol
  Acebutolol
• Propranolol Carteolol Esmolol
  (Practolol)
• Timolol Penbutolol Metoprolol
  Celiprolol
• Sotalol Alprenolol Bevantolol
• Tertalolol Oxprenolol Bisoprolol
• Dilevalol
  Betaxolol

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VASODILATORS

• Direct
• Hydralazine A lt V
• Minoxidil A lt V
• Nitroproside A lt v
• Diazoxide A lt V
• Nitroglycerin V lt A
• Calcium Blockers A lt V
• Converting Enz. Inh. A lt V
• Alpha Blockers A V

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Pharmacological Effects of Ca Blockers
Deltiazem Verapamil Nefidipine Nicardipine
Heart rate - -
Myocardial Contractility - -
Nodal Conduction - -
Peripheral Vasodilation
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ACE INHIBITORS

• Captopril
• Enalipril
• Lisinopril
• Fosinopril
• Ramipril
• Quinapril
• Benazepril
• ANGIOTENSION II ANTAGONIST
• losartan
• Olmesartan

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DRUGS COMMONLY USED
B-Blockers In-patient with angina pectoris Or Ca Channel Blockers Peripheral Vascular Disease
ACE Inhibitor In-patient with DM Or Ca Blocker In patient with hyperlipidemia
Diuretics In CHF Or ACE Inhibitors
Diuretics In CRF Or Ca Blockers
Diuretics Or Ca Blockers In Asthma COPD
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TABLE 29-12 PARENTERAL DRUGS FOR TREATMENT OF
HYPERTENSIVE EMERGENCY (IN ORDER OF RAPIDITY OF
ACTION)
DRUG DOSAGE ONSET OF ACTION ADVERSE EFFECTS
VASODILATORS Nitroprusside (Nipride,Nitropress) 0.25 -10 ug/kg/min as I.V. infusion Instantaneous Nausea, vaomiting, muscle twitching sweating, thiocyanate intoxication
Nitroglycerin 5 -100 ug/min as I.V. Infusion 2 5 min Tachycardia, flushing, headache, vomiting, methemoglobinemia
Diazoxide (Hyperstat) 50 100 mg/IV bolus, repeated or 15 30 mg/min by I.V infusion 2 4 min Nausea, hypotension, flushing, tachycardia, chest pain
Hydralazine (Apresoline) 10 20 mg I.V 10 50 mg I.M 10 20 min 20 30 min Tachycardia, flushing, headache, vomiting, aggravation of angina
Enalapril (Vasotec IV) 1.25 5 mg q 6 hr 15 min Precipitous fall in BP in high renin states response variable
Nicardiprine 5 15 mg/hr I.V 10 min Tachycardia, headache, flushing, local phlebitis

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TABLE 29-12 PARENTERAL DRUGS FOR TREATMENT OF
HYPERTENSIVE EMERGENCY (IN ORDER RAPIDITY OF
ACTION)(Cont.)
DRUG DOSAGE ONSET OF ACTION ADVERSE EFFECTS
ADRENERGIC INHIBITORS
Phentolamine (Regitine) 5 15 mg I.V. 1 2 min Tachycardia, flushing
Trimethaphan (Arfonad) 0.5 5 mg/min as I.V. infusion 1 5 min Paresis of bowel and bladder, orthostatic hypotension, blurred vision, dry mouth
Esmolol ( Brevibloc) 500 ug/kg/min for 4 min, then 150 -300 ug/kg/min I.V. 1 2 min Hypotension
Propranolol (Inderal) 1 10 mg load 3ng/hr 1 2 min Beta blocker side effects, e.g., bronchospasm, decreased cardiac output
Laberalol (Normodyne, Trandate) 2080 mg I.V. bolus every 10 min 2 mg/min I.V. infusion 5 10 min Vomiting, scalp tingling, burning in throat, postural hypotension, dizziness, nausea
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Table 9 35 Adverse Effects of Antihypertensive
Agents
Diuretics Nausea, muscle cramps, hypovolemia, hypokalemia, hyponatremia, hyperurcemia, hyperglycemia, rash.
Potassium-sparing diuretics Hyperkalemia, gynecomastia
Adrenergic inhibitors Methyldopa Drowsiness, dry mouth, impotence, hepatitis, postural hypotension, hemolytic anemia, fever
Reserpine Somnolence, nasal congestion, nightmares, mental depression
Gunethidine Postural hypotension, diarrhea, retrograde ejaculation, weakness on exertion
Propranolol Bradycardia, left ventricular failure, asthma, Raynauds syndrome, central nervous system symptoms, sodium retention
Mecamylamine and trimethaphan Postural hypotension, parasympathetic blockade with constipation and paralytic ileus, loss of visual accommodation.
Clonidine Dry mouth, drowsiness, rebound hypertension if drug stopped abruptly
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Table 9 35 Adverse Effects of Antihypertensive
Agents(Cont.)
vasodilator agents Prazosin Tachycardia, headache, postural weakness and hypotension
Hydralazine Lupuslike syndrome, headache, tachycardia, angina
Minoxidil Tachycardia, hirsutism, headache, sodium retention
Diazoxide Hyperglycemia, tachycardia, angina, sodium retention
Sodium nitroprusside Excess hypotension, acute tubular necrosis, thiocyanate toxicity